专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-3694472-A 优先权日:1970-05-12 标题 :Synthesis of pyrethric acid 发明人:MARTEL JACQUES; BUENDIA JEAN 权利人:ROUSSEL UCLAF 摘要:BY REACTING 3,3-DIMETHYL-2-FORMYL-1-CYCLOPROPANECARBOXYLIC (1R, 2R) acid or a salt thereof with methyl propionate under anhydrous basic conditions. A novel process for the preparation of 3,3-dimethyl-2-(2''methoxycarbonyl-trans 1''-propenyl)-1-cyclopropane carboxylic (1R, 2R) acid or d-trans pyrethric (1R,2R) acid of the formula
专利号:WO-9618592-A1 优先权日:1994-12-10 标 题:Resin-bound phosphonium salts and their use in organic synthesis 发明人:HUGHES IAN 权利人:SMITHKLINE BEECHAM PLC; HUGHES IAN 摘要:The invention relates to carrying out organic chemistry on a solid support, and in particular to the use of a phosphonium salt as a linker for solid phase synthesis.
专利号:WO-2011121091-A1 优先权日:2010-03-31 标题:Efficient synthesis for the preparation of montelukast and novel crystalline form of intermediates therein 发明人:KIDEMET DAVOR; BOGDAN STEFANE; KLJAJIC ALEN; BENKIC PRIMOZ; STROPNIK TADEJ; PLAPER IGOR 权利人:KRKA D D NOVO MESTO; KIDEMET DAVOR; BOGDAN STEFANE; KLJAJIC ALEN; BENKIC PRIMOZ; STROPNIK TADEJ; PLAPER IGOR 摘要:The present invention describes the improved process for the preparation of montelukast acid (VII) and its pharmaceutically acceptable salts and esters using a novel synthesis step. The process is cost effective, environment friendly, and easily scale up to commercial level and leads to products having high chemical and optical purity. Moreover, the present invention provides a novel crystalline intermediate (IV) that is useful in this process and a method for its production. In a further aspect, the process of the present invention includes a step of removing ketone by-products be derivatization.
专利号:US-2014051854-A1 优先权日:2010-07-26 标题 :Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof
专利号:US-4950660-A 优先权日:1987-09-07 标 题:Beta-lactam compound and process for production thereof 发明人:ATSUMI KUNIO; YAMAMOTO YUICHI; SAKAGAMI KENJI; NISHIHATA KEN; KONDO SHINICHI 权利人:MEIJI SEIKA CO 摘要:The present invention relates to a cephem compound of formula (III) shown in the description. The compound is useful as an intermediate for the synthesis of beta -lactam antibiotics of new class and also to a process for producing the same. The cephem compound (III) is produced by reacting a cephem compound of formula (I) with a nitrogen-containing compound of formula (II) under acid-capturing conditions. The process can be performed easily under mild conditions.
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合成参考文献
参考文献:10.1002/rcm.654 摘要:Gouw JW, Burgers PC, Trikoupis MA, Terlouw JK. Derivatization of small oligosaccharides prior to analysis by matrix-assisted laser desorption/ionization using glycidyltrimethylammonium chloride and Girard's reagent T. Rapid Commun Mass Spectrom. 2002;16(10):905–12. doi: 10.1002/rcm.654. 参考文献:10.1016/j.saa.2006.02.063 摘要:Mostafa MM. Spectroscopic studies of some thiosemicarbazide compounds derived from Girard's T and P. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy. 2007 Feb;66(2):480–6. doi: 10.1016/j.saa.2006.02.063.